Information on EC 2.7.1.32 - choline kinase

2-aminoethanol + ATP

ADP + 2-aminoethyl phosphate

-

641357

Substrates: -
Products: -

?

2-methylaminoethanol + ATP

ADP + 2-methylaminoethyl phosphate

-

641357

Substrates: -
Products: -

?

ATP + choline

ADP + O-phosphocholine

55 entries

ATP + choline

ADP + phosphocholine

32 entries

ATP + dimethylethanolamine

ADP + phosphodimethylethanolamine

-

Substrates: -
Products: -

?

ATP + ethanolamine

ADP + ethanolamine phosphate

ATP + ethanolamine

ADP + O-phosphoethanolamine

ATP + ethanolamine

ADP + phosphoethanolamine

-

Substrates: -
Products: -

?

beta-methylcholine + ATP

ADP + beta-methylcholine phosphate

-

Substrates: -
Products: -

?

choline + ATP

O-phosphocholine + ADP

choline + ATP

phosphocholine + ADP

6 entries

choline + ATP

phosphorylcholine + ADP

Histophilus somni

B0URY8

705538

Substrates: -
Products: -

?

CTP + choline

CDP + choline phosphate

-

641371

Substrates: 12% of the activity with ATP
Products: -

?

diethanolamine + ATP

ADP + O-phospho-diethanolamine

-

Substrates: -
Products: -

?

ethanolamine + ATP

ADP + ethanolamine phosphate

ethanolamine + ATP

O-phosphoethanolamine + ADP

-

Substrates: first step in the biosynthesis of the glycerophospholipid glycerophosphoethanolamine
Products: -

?

ethanolamine + ATP

phosphoethanolamine + ADP

706447

Substrates: -
Products: -

?

GTP + choline

GDP + choline phosphate

N,N,N-triethylethanolamine + ATP

ADP + N,N,N-triethylethanolamine phosphate

-

641363

Substrates: weak
Products: -

?

N,N-diethyl-N-methylethanolamine + ATP

ADP + N,N-diethyl-N-methylethanolamine phosphate

-

641363

Substrates: weak
Products: -

?

N,N-diethylethanolamine + ATP

ADP + N,N-diethylethanolamine phosphate

N,N-diethylethanolamine + ATP

ADP + O-phospho-N-diethylethanolamine

-

Substrates: -
Products: -

?

N,N-diisopropylethanolamine + ATP

ADP + N,N-diisopropylethanolamine phosphate

-

Substrates: -
Products: -

?

N,N-dimethyl-N-propylethanolamine + ATP

ADP + N,N-dimethyl-N-propylethanolamine phosphate

-

641363

Substrates: -
Products: -

?

N,N-dimethylaminopropanol + ATP

ADP + N,N-dimethylaminopropyl phosphate

-

Substrates: -
Products: -

?

N,N-dimethylethanolamine + ATP

ADP + N,N-dimethylethanolamine phosphate

N,N-dimethylethanolamine + ATP

ADP + O-phospho-N,N-dimethylethanolamine

-

Substrates: -
Products: -

?

N,N-dimethylethylcholine + ATP

ADP + N,N-dimethylethylcholine phosphate

-

Substrates: -
Products: -

?

N,N-dimethylisopropylcholine + ATP

ADP + N,N-dimethylisopropylcholine phosphate

-

Substrates: -
Products: -

?

N,N-dimethylpropylcholine + ATP

ADP + N,N-dimethylpropylcholine phosphate

-

Substrates: -
Products: -

?

N-ethylethanolamine + ATP

ADP + O-phospho-N-ethylethanolamine

-

Substrates: -
Products: -

?

N-methylethanolamine + ATP

ADP + N-methylethanolamine phosphate

N-methylethanolamine + ATP

ADP + O-phospho-N-methylethanolamine

-

Substrates: -
Products: -

?

N-monoethylethanolamine + ATP

ADP + N-monoethylethanolamine phosphate

-

641351

Substrates: -
Products: -

?

N-monomethylethanolamine + ATP

ADP + N-monomethylethanolamine phosphate

UTP + choline

UDP + choline phosphate

additional information

?

-

ATP + choline

ADP + O-phosphocholine

ATP + choline

ADP + phosphocholine

19 entries

choline + ATP

O-phosphocholine + ADP

-

Substrates: first step in the biosynthesis of the glycerophospholipid glycerophosphocholine
Products: -

?

choline + ATP

phosphocholine + ADP

ethanolamine + ATP

O-phosphoethanolamine + ADP

-

Substrates: first step in the biosynthesis of the glycerophospholipid glycerophosphoethanolamine
Products: -

?

additional information

?

-

-

685941

Substrates: microarray analysis detected changes in the expression of 33 proliferation-related genes with Chk down-regulation
Products: -

?

ATP

19 entries

Ca2+

6 entries

Carpronium chloride

-

stimulates

Chlorocholine chloride

-

stimulates

K+

Li+

-

stimulates

Mg2+

37 entries

MgCl2

-

assay at

Mn2+

Na+

NH4+

-

stimulates

additional information

(1-azabicyclo[2.2.2]octan-3-yl)bis(5-chlorothiophen-2-yl)methanol

(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol

(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone

-

(azepan-1-yl)(piperazin-1-yl)methanone

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[(4-dimethylamino)pyridinium] tribromide

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(3,5-dichloro-N-methylanilino)pyridinium] tribromide

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(4-chloro-N-methylanilino)pyridinium] tribromide

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(N-methylanilino)pyridinium] tribromide

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(piperidino)pyridinium] tribromide

-

1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(pyrrolidino)pyridinium] tribromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(3-hydroxyquinuclidinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)pyridinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)-7-chloroquinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(methyl(phenyl)amino)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(pyrrolidin-1-yl)pyridinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(methyl(phenyl)amino)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(pyrrolidin-1-yl)quinolinium) bromide

-

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(quinuclidinium) bromide

-

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

-

IC50: 0.0528 mM

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

-

IC50: 0.0842 mM

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0084 mM

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0072 mM

1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

-

IC50: 0.0375 mM

1,1'-(benzene-1,3-diylmethylene)bis[(4-dimethylamino)pyridinium] dibromide

-

1,1'-(benzene-1,3-diylmethylene)bis[4-(N-methylanilino)pyridinium] dibromide

-

1,1'-(benzene-1,3-diylmethylene)bis[4-(piperidino)pyridinium] dibromide

-

1,1'-(benzene-1,3-diylmethylene)bis[4-(pyrrolidino)pyridinium] dibromide

-

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

-

IC50: 0.0377 mM

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

-

IC50: 0.024 mM

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0097 mM

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0029 mM

1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

-

IC50: 0.015 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide

-

IC50: 0.0119 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide

-

IC50: 0.0206 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide

-

IC50: 0.0012 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide

-

IC50: 0.0005 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

-

IC50: 0.0019 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

-

IC50: 0.0058 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0026 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0015 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.0021 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

-

IC50: 0.147 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

-

IC50: 0.0012 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.0057 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.0044 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide

-

IC50: 0.0013 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

-

IC50: 0.00043 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0004 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0568 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.0096 mM

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0031 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide

-

IC50: above 0.2 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide

-

IC50: 0.0633 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide

-

IC50: 0.0811 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide

-

IC50: 0.0022 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

-

IC50: 0.0088 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

-

IC50: 0.0111 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0034 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0018 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.002 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

-

IC50: 0.0461 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

-

IC50: 0.0198 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.0114 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.0397 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide

-

IC50: 0.0178 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

-

IC50: 0.0043 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.003 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0961 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.0206 mM

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0114 mM

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)

-

1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)

-

1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)

-

1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)

-

1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)

-

1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

-

1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)

-

1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)

-

1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)

-

1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)

-

1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

-

1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

-

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

-

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide

-

IC50: 0.098 mM

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide

-

IC50: above 0.1 mM

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

-

IC50: 0.0482 mM; IC50: above 0.1 mM

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide

-

IC50: above 0.1 mM

1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide

-

IC50: above 0.2 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide

-

IC50: 0.08 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide

-

IC50: 0.006 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.0048 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

-

IC50: 0.0575 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

-

IC50: 0.001 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

-

IC50: 0.0057 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.0102 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide

-

IC50: 0.0023 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0014 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.133 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

-

IC50: 0.009 mM

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

-

IC50: 0.0035 mM

1,1'-[[1,1'-biphenyl]-4,4'-diylbis(methylene)]bis[4-[(4-chlorophenyl)(methyl)amino]quinolin-1-ium]

1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane

-

1-(4-(4-[(3-aminophenoxy)methyl]phenethyl)benzyl)-4-(dimethylamino)pyridinium bromide

21.9% inhibition at 0.05 mM

1-(4-[4-[(3-hydroxyphenylamino)methyl]phenethyl]-benzyl)-4-(pyrrolidin-1-yl)pyridinium bromide

13.6% inhibition at 0.05 mM

1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide

0.1% inhibition at 0.01 mM, 24.8% inhibition at 0.05 mM

1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide

62.3% inhibition at 0.01 mM, 71.4% inhibition at 0.05 mM

1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-(dimethylamino)pyridinium bromide

38.6% inhibition at 0.01 mM, 81% inhibition at 0.05 mM

1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide

28.6% inhibition at 0.01 mM, 46.9% inhibition at 0.05 mM

1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide

37.6% inhibition at 0.01 mM, 51% inhibition at 0.05 mM

1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-pyrrolidinopyridinium bromide

50.2% inhibition at 0.01 mM, 72.8% inhibition at 0.05 mM

1-([4'-[(3-aminophenoxy)methyl]biphenyl-4-yl]methyl)-4-(dimethylamino)pyridinium bromide

79.8% inhibition at 0.05 mM

1-([4'-[(3-aminophenoxy)methyl]biphenyl-4-yl]methyl)-4-(pyrrolidin-1-yl)pyridinium bromide

20.8% inhibition at 0.05 mM

1-([4'-[(3-hydroxyphenylamino)methyl]biphenyl-4-yl]-methyl)-4-(pyrrolidin-1-yl)-pyridinium bromide

28.2% inhibition at 0.05 mM

1-([4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

-

1-([4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-([4-[(6-amino-9H-purin-9-yl)methyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

-

1-([4-[(6-amino-9H-purin-9-yl)methyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

-

1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

-

1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane

-

1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane

-

1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane

-

1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(dimethylamino)pyridin-1-ium bromide

-

1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-[(4-[4-[4-([4-[(4-chlorophenyl)(methyl)amino]pyridin-1-ium-1-yl]methyl)phenyl]butyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium

-

1-[(4-[4-[4-([4-[(4-chlorophenyl)(methyl)amino]pyridin-1-ium-1-yl]methyl)phenyl]butyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium dibromide

-

1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium bromide

-

1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-[4'-[(6-amino-9H-purin-9-yl)methyl][1,1'-biphenyl]-4-yl]-4-(dimethylamino)pyridin-1-ium bromide

-

1-[4-(4-[4-[(3-aminophenoxy)methyl]phenyl]butyl)-benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide

21.6% inhibition at 0.05 mM

1-[4-(4-[4-[(3-hydroxyphenylamino)methyl]phenyl]-butyl)benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide

18% inhibition at 0.05 mM

1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide

61.3% inhibition at 0.01 mM, 68.2% inhibition at 0.05 mM

1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide

22.6% inhibition at 0.01 mM, 59.9% inhibition at 0.05 mM

1-[4-(4-[4-[(6-amino-9H-purin-8-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide

Helicobacter pylori

-

721292

1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide

66.7% inhibition at 0.01 mM, 89.7% inhibition at 0.05 mM

1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide

36.9% inhibition at 0.01 mM, 41.9% inhibition at 0.05 mM

1-[4-[(3-aminophenoxy)methyl]benzyl]-4-(dimethylamino)pyridinium bromide

37.7% inhibition at 0.05 mM

1-[4-[(3-aminophenoxy)methyl]benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide

12.9% inhibition at 0.05 mM

1-[4-[(3-hydroxyphenylamino)methyl]benzyl]-4-(pyrrolidin-1-yl)pyridinium bromide

41.3% inhibition at 0.05 mM

1-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]methanamine

analysis of the enzyme bound structure, PDB ID 5EQE

1-[4-[(6-amino-3H-purin-3-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide

25% inhibition at 0.01 mM, 50.2% inhibition at 0.05 mM

1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide

46.7% inhibition at 0.01 mM, 54.1% inhibition at 0.05 mM

1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-pyrrolidinopyridinium bromide

27% inhibition at 0.05 mM

1-[[4-(2-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]ethyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide

-

1-[[4-(2-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]ethyl)phenyl]methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide

-

739680, 759713

1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

-

1-[[4-[4-[[4-(4-chloro-N-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-N-(4-chlorophenyl)-N-methylquinolin-1-ium-4-amine

i.e. TCD-717 or RSM-932A, strong inhibition of ChoKalpha, TCD-717 does not bind directly in the choline pocket but rather in a proximal location near the surface of the enzyme. Most notably, residues Tyr148, Ala176, Met177, Glu180, Phe200, Pro201, Trp248, Thr252, Tyr256, Glu332, Tyr333, Phe341, and Leu419 serve to orient and hold TCD-717 in place. Interaction of TCD-717 with ChoKalpha is driven by hydrophobic interactions across the N- and C-terminal domains. Binding of TCD-717 induces conformational changes compared to the unbound ChoKalpha structure. TCD-717 has completed phase I clinical trials

12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide

-

IC50: 0.0132 mM

12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide

-

IC50: 0.0021 mM

14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide

2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile

-

2-amino-1-butanol

-

3-Trimethylammonio-1-propanol

-

4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazol

-

-

4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)

-

4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)

-

4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)

-

4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)

-

4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl

-

4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile

-

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-[4-[(4-dimethylaminopyridinium-1-yl)methyl]benzyl]pyridinium dibromide

-

4-(4-chloro-N-methylanilino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]benzyl]pyridinium dibromide

-

4-(dimethylamino)-1-(4-(3-(4-(((3-hydroxyphenyl)amino)methyl)phenyl)propyl)benzyl)pyridin-1-ium bromide

12.9% inhibition at 0.05 mM

4-(dimethylamino)-1-(4-(4-(((3-hydroxyphenyl)amino)methyl)benzyl)benzyl)pyridin-1-ium bromide

39.5% inhibition at 0.05 mM

4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenethyl]benzyl)pyridinium dibromide

-

4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]benzyl)pyridinium dibromide

-

4-(dimethylamino)-1-({4-[(3-hydroxyphenylamino)-methyl]biphenyl-4-yl}methyl)pyridinium bromide

66.2% inhibition at 0.05 mM

4-(dimethylamino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]butyl)benzyl]pyridinium dibromide

-

4-(dimethylamino)-1-[4-[(3-hydroxyphenylamino)-methyl]benzyl]pyridinium bromide

52.4% inhibition at 0.05 mM

4-(dimethylamino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]-benzyl]pyridinium dibromide

-

4-chloro-N-methylanilino

-

IC50: 0.0014 mM

4-[(4-chlorophenyl)(methyl)amino]-1-[(4'-[[4-(dimethylamino)phenyl]methyl][1,1'-biphenyl]-4-yl)methyl]pyridin-1-ium bromide

-

5'-dithio-bis-(2-nitrobenzoic acid)

-

modest inhibitory activity

5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide

-

IC50: 0.0248 mM

5,5'-dithiobis(2-nitrobenzoic acid)

5-fluorouracil

-

Investigation of the effect of combining transient siRNA-chk transfection with the anticancer drug 5-fluorouracil on cell viability and proliferation. Choline kinase down-regulation with 5-fluorouracil treatment increased cell kill in cancer cells.

685941

6-(trifluoromethyl)pyrimidin-4-amine

-

6-amino-3-([4-[4-(4-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl]phenyl)butyl]phenyl]methyl)-9H-purin-3-ium

-

6-amino-3-([4-[4-(4-[[4-(pyrrolidin-1-yl)pyridin-1-ium-1-yl]methyl]phenyl)butyl]phenyl]methyl)-9H-purin-3-ium

-

6-amino-3-[(4'-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-9H-purin-3-ium

-

758809, 759713

6-amino-3-[(4-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl]phenyl)methyl]-9H-purin-3-ium

-

6-[(1-methyl-1,4-diazepan-6-yl)methyl]quinoline

-

7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone

-

7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium

-

Acetylcholine

adenosine

ADP

AMP

ATP

betaine

-

Ca2+

choline

Choline analogues

choline kinase inhibitor Mn58b

-

choline kinase inhibitor TCD828

-

705667

-

choline phosphate

-

citrate

-

Cu2+

-

cyclophane

-

Cytidine diphosphocholine

-

Diethylmethylcholine

-

dimethylethanolamine

-

EDTA

about 10% residual activity at 5 mM

ethanolamine

6 entries

H-89

-

no activity on choline kinase at 5 mM ATP, decreasing the ATP concentration to 100 microM has no effect on choline kinase

HC-3

hemicholinium

hemicholinium-3

hemicolinium

-

hexadecyltrimethylammonium bromide

-

60% inhibition at 0.1 mM; HDTAB, structural resemblance to hexadecylphosphocholine, exhibits an antimalarial effect and inhibits choline kinase in a dose-dependent manner. For purified protein: 60% inhibition at 100 microM (in presence of 250 microM choline), 60% inhibition at 50 microM (in presence of 100 microM choline). HDTAB may compete with choline for the choline binding site of choline kinase and may offer competitive inhibition with respect to choline. The concentration of HDTAB required to inhibit Plasmodium falciparum growth by 62% was 10times lower than the concentration required to inhibit purified choline kinase by 60% in vitro

KF

methionine

methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate

-

MgADP-

-

MN58b

N,N,N-trimethyl-N-(5,5-diphenylpent-4-en-1-yl)ammonium iodide

-

N,N,N-trimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide

-

N-(3,5-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide

CK37, identified through computational virtual screening, inhibits ChoKalpha activity both in enzymatic and in cellular assays, is able to suppress pCho production and tumor growth in vivo

N-ethylmaleimide

N-iodomethyl-N,N-dimethyl-N-(4,4-diphenylbut-3-en-1-yl)ammonium iodide

-

N-iodomethyl-N,N-dimethyl-N-(5,5-diphenylpent-4-en-1-yl)ammonium iodide

-

N-iodomethyl-N,N-dimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide

-

N-iodomethylcholine iodide

-

N-Methyl-N,N-diisopropylethanolamine

-

641350

N-Methyl-N-isopropylethanolamine

-

641350

N-[2-bromocinnamyl(amino)ethyl]-5-isoquinoline sulfonamide

-

NaCl

-

8.7-35 mM: slight activation, 70 mM: inactivation

o-phenanthroline

Lathyrus oleraceus

-

641380

p-chloromercuribenzoate

-

641358

p-hydroxymercuribenzoate

Chlorocebus aethiops

-

641369

phosphocholine

-

40% and 66% inhibition at 2.5 mM and 10 mM, respectively

phosphorylcholine

physostigmine

-

piperazine

-

modest inhibitory activity

purinyl-6-histamine

-

modest inhibitory activity

Quinacrine

-

indirect inhibitor

RSM-932A

dysregulates the production of LTA, distorts the cell wall, and affects cell sensitivity to deoxycholate induced autolysis

RSM932A

also called TCD-717

SAR97276

-

serine

stearoyl-CoA

Triethanolammonio-1-choline

-

V-11-023907

-

[4-(4-methyl-1,4-diazepan-1-yl)phenyl]methanol

-

additional information

-

2-Chloroethylammonium chloride

Phaseolus vulgaris

-

stimulates

641356

Acetylcholine

-

stimulates

atropine

Phaseolus vulgaris

-

stimulates

641356

c-Src

isoform CHKA2 total cellular activity and protein levels are regulated by c-Src

-

carbon tetrachloride

Choline esters

-

activate

641357

cysteine

-

omission of cysteine decreases the reaction rate by 40%

641351

epidermal growth factor receptor

isoform CHKA2 total cellular activity and protein levels are regulated by epidermal growth factor receptor. In the presence of co-transfected epidermal growth factor receptor, the activity of wild type isoform CHKA2 is increased 2.5 fold

-

gibberellic acid

Phaseolus vulgaris

-

stimulates

641356

isopropyl-beta-D-thiogalactoside

-

recombinant protein expression is induced with 1 mM

putrescine

-

slight stimulation

spermidine

-

stimulates

spermine

Zinc

-

intacellular zinc depletion resulted in a concentration-dependent induction of CKI1 expression

687686

additional information

-

0.0206 - 45

ATP

50 entries

0.444

beta-Methylcholine

0.002 - 13

choline

64 entries

0.94

dimethylethanolamine

-

in 100 mM Tris-HCl (pH 8.5), at 37°C

0.787 - 75

ethanolamine

11 entries

0.025

N,N-diethylethanolamine

0.4

N,N-Diisopropylethanolamine

0.208

N,N-Dimethylaminopropanol

0.022 - 0.085

N,N-dimethylethanolamine

0.118 - 3.7

N-Monomethylethanolamine

additional information

ethanolamine

21 entries

4.5 - 54.39

ATP

0.24 - 130

choline

45 entries

83.69 - 86.24

ATP

24.15 - 114.9

choline

0.124 - 0.182

1,1'-[butane-1,4-diylbis[(4,1-phenylene)methylene]]bis[4-(dimethylamino)pyridin-1-ium]

0.0106 - 0.0358

1,1'-[[1,1'-biphenyl]-4,4'-diylbis(methylene)]bis[4-[(4-chlorophenyl)(methyl)amino]quinolin-1-ium]

0.014

choline

-

pH 8.5, 37°C

641370

2 - 5.5

ethanolamine

0.00021 - 0.116

hemicholinium-3

7 entries

3.45

phosphocholine

-

in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37°C

0.9 - 1.03

SAR97276

additional information

-

0.00002

(1S)-1-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-3-[2-[(oxan-4-yl)oxy]phenyl]-1-phenylpropan-1-ol

Homo sapiens

pH 7.0, 25°C, recombinant enzyme

0.000251

(4-methyl-1,4-diazepan-1-yl)(4'-((4-methyl-1,4-diazepan-1-yl)-methyl)-[1,1'-biphenyl]-4-yl)methanone

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.00951

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(3-hydroxyquinuclidinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00163

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)pyridinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00327

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00202

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)-7-chloroquinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00166

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(azepan-1-yl)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.001

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00685

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(methyl(phenyl)amino)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00956

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(4-(pyrrolidin-1-yl)pyridinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.01622

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-((4-chlorophenyl)(methyl)amino)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00279

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(methyl(phenyl)amino)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.00092

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(7-chloro-4-(pyrrolidin-1-yl)quinolinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.03754

1,1'-(((ethane-1,2-diylbis(oxy))bis(4,1-phenylene))bis(methylene))bis(quinuclidinium) bromide

Homo sapiens

at pH 8.5 and 37°C

0.0528

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0528 mM

0.0842

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0842 mM

0.0084

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0084 mM

0.0072

1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0072 mM

0.0375

1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

Homo sapiens

-

IC50: 0.0375 mM

0.0377

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0377 mM

0.024

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.024 mM

0.0097

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0097 mM

0.0029

1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0029 mM

0.015

1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

Homo sapiens

-

IC50: 0.015 mM

0.0119

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0119 mM

0.0206

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide

Homo sapiens

-

IC50: 0.0206 mM

0.0012

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide

Homo sapiens

-

IC50: 0.0012 mM

0.0005

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0005 mM

0.0019

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0019 mM

0.0058

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0058 mM

0.0026

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0026 mM

0.0015

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0015 mM

0.0021

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.0021 mM

0.147

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

Homo sapiens

-

IC50: 0.147 mM

0.0012

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0012 mM

0.0057

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.0057 mM

0.0044

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0044 mM

0.0013

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0013 mM

0.00043

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

Homo sapiens

-

IC50: 0.00043 mM

0.0004

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0004 mM

0.0568

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0568 mM

0.0096

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0096 mM

0.0031

1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0031 mM

0.2

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide

Homo sapiens

-

IC50: above 0.2 mM

0.0633

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide

Homo sapiens

-

IC50: 0.0633 mM

0.0811

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide

Homo sapiens

-

IC50: 0.0811 mM

0.0022

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0022 mM

0.0088

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0088 mM

0.0111

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.0111 mM

0.0034

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0034 mM

0.0018

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide

Homo sapiens

-

IC50: 0.0018 mM

0.002

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.002 mM

0.0461

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0461 mM

0.0198

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0198 mM

0.0114

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.0114 mM

0.0397

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0397 mM

0.0178

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0178 mM

0.0043

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide

Homo sapiens

-

IC50: 0.0043 mM

0.003

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.003 mM

0.0961

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0961 mM

0.0206

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0206 mM

0.0114

1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0114 mM

0.08

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)

Homo sapiens

-

0.0006

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)

Homo sapiens

-

0.0102

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0023

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]

Homo sapiens

-

0.0048

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.0014

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.0575

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

Homo sapiens

-

0.133

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.009

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0057

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.0035

1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.01109

1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)

Homo sapiens

-

0.0206

1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)

Homo sapiens

-

0.0012

1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)

Homo sapiens

-

0.0005

1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)

Homo sapiens

-

0.0012

1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)

Homo sapiens

-

0.0044

1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0013

1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]

Homo sapiens

-

0.0021

1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.0004

1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.147

1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

Homo sapiens

-

0.0568

1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.0096

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0057

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.0031

1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.0633

1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)

Homo sapiens

-

0.0811

1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)

Homo sapiens

-

0.0022

1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)

Homo sapiens

-

0.0198

1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)

Homo sapiens

-

0.0397

1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0178

1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]

Homo sapiens

-

0.002

1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.003

1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.0461

1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]

Homo sapiens

-

0.0961

1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.0206

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]

Homo sapiens

-

0.0114

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]

Homo sapiens

-

0.0114

1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]

Homo sapiens

-

0.098

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: 0.098 mM

0.1

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide

Homo sapiens

-

IC50: above 0.1 mM

0.0482 - 0.1

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide

0.1

1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide

Homo sapiens

-

IC50: above 0.1 mM

0.2

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide

Homo sapiens

-

IC50: above 0.2 mM

0.08

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide

Homo sapiens

-

IC50: 0.08 mM

0.006

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.006 mM

0.0048

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.0048 mM

0.0575

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide

Homo sapiens

-

IC50: 0.0575 mM

0.001

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide

Homo sapiens

-

IC50: 0.001 mM

0.0057

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide

Homo sapiens

-

IC50: 0.0057 mM

0.0102

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0102 mM

0.0023

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.0023 mM

0.0014

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0014 mM

0.133

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.133 mM

0.009

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide

Homo sapiens

-

IC50: 0.009 mM

0.0035

1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide

Homo sapiens

-

IC50: 0.0035 mM

0.00143

1-((4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-4-methyl-1,4-diazepane

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.00621

1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide

Homo sapiens

in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C

0.00232

1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.01836

1-([4-[2-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)ethyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.01883

1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(dimethylamino)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.05

1-([4-[4-(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)butyl]phenyl]methyl)-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

Homo sapiens

above, pH and temperature not specified in the publication, recombinant ChoKalpha

0.0013 - 0.0015

1-methyl-4-((4'-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-4-yl)-methyl)-1,4-diazepane

0.0026

1-methyl-4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-1,4-diazepane

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0026

1-methyl-4-(naphthalen-2-ylmethyl)-1,4-diazepane

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0015

1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(dimethylamino)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.05

1-[(4'-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl][1,1'-biphenyl]-4-yl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

Homo sapiens

above, pH and temperature not specified in the publication, recombinant ChoKalpha

0.0004

1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(dimethylamino)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.00791

1-[(4-[[6-(benzylsulfanyl)-9H-purin-9-yl]methyl]phenyl)methyl]-4-(pyrrolidin-1-yl)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.0389

1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide

Homo sapiens

in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C

0.0107

1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide

Homo sapiens

in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37°C

0.087

1-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]methanamine

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0107

1-[[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)phenyl]methyl]-4-(dimethylamino)pyridin-1-ium bromide

Homo sapiens

pH and temperature not specified in the publication, recombinant ChoKalpha

0.00052

1-[[4-[4-[[4-(4-chloro-N-methylanilino)quinolin-1-ium-1-yl]methyl]phenyl]phenyl]methyl]-N-(4-chlorophenyl)-N-methylquinolin-1-ium-4-amine

Homo sapiens

wild-type enzyme ChoKalpha, pH 7.5, 37°C

0.0132

12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide

Homo sapiens

-

IC50: 0.0132 mM

0.0021

12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide

Homo sapiens

-

IC50: 0.0021 mM

0.0003

14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide

0.000085

2'-fluoro-4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

3.2

2-amino-1-butanol

Plasmodium falciparum 3D7

endogenous enzyme

0.000233

4,4'-((2,3-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.000165

4,4'-((2-fluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.000255

4,4'-((3,5-difluoro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis-(1-methyl-1,4-diazepane)

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.000268

4,4'-((3-chloro-[1,1'-biphenyl]-4,4'-diyl)bis(methylene))bis(1-methyl-1,4-diazepane)

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.000457

4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-1,1'-biphenyl

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.000066

4,4'-bis((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0007

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0015

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0025

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenethyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0022

4-(4-chloro-N-methylanilino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0012

4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-dimethylaminopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0015

4-(4-chloro-N-methylanilino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]phenyl]butyl)benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0009

4-(4-chloro-N-methylanilino)-1-[4-[(4-dimethylaminopyridinium-1-yl)methyl]benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0006

4-(4-chloro-N-methylanilino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0012

4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenethyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0008

4-(dimethylamino)-1-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]benzyl)pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0009

4-(dimethylamino)-1-[4-(4-[4-[(4-pyrrolidinopyridinium-1-yl)-methyl]phenyl]butyl)benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.008

4-(dimethylamino)-1-[4-[(4-pyrrolidinopyridinium-1-yl)methyl]-benzyl]pyridinium dibromide

Homo sapiens

at pH 8.5 and 37°C

0.0014

4-chloro-N-methylanilino

Homo sapiens

-

IC50: 0.0014 mM

0.0248

5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide

Homo sapiens

-

IC50: 0.0248 mM

0.0172

6-[(1-methyl-1,4-diazepan-6-yl)methyl]quinoline

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0039

7-((4-methyl-1,4-diazepan-1-yl)methyl)quinolone

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.001

7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium

Homo sapiens

-

0.005 - 0.1075

choline kinase inhibitor Mn58b

-

0.057 - 2.7

hemicholinium-3

0.00495

methyl 4'-((4-methyl-1,4-diazepan-1-yl)methyl)-[1,1'-biphenyl]-4-carboxylate

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

0.0001 - 0.197

MN58b

21 entries

0.0005

RSM-932A

Streptococcus pneumoniae

pH and temperature not specified in the publication

0.00192

RSM932A

Homo sapiens

at pH 8.5 and 37°C

0.52 - 1.12

SAR97276

0.00047

V-11-023907

Homo sapiens

in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25°C

721743

2

[4-(4-methyl-1,4-diazepan-1-yl)phenyl]methanol

Homo sapiens

pH 7.5, 25°C, recombinant enzyme

additional information

Homo sapiens

IC50 values for inhibitors with HepG2 cell and the cytosolic fraction of HepG2 cells, overview

-

0.000139

-

skeletal muscle, hindlimbs of +/+ CK-alpha mice, supernatant of tissue homogenates are incubated in volume of 0.100 ml of reaction buffer at 37°C for 30 min. The reaction product, phosphocholine, is separated using an AG1-X8 column.To determine the activity of each CK isoform, supernatant fractions are treated with an antisera raised against GST (control), GST-CK-alpha or GST-CK-beta fusion proteins combined with protein A-Sepharose overnight at 4°C, and the supernatant is used.

687709

0.000484

-

in 40 mM Tris/HCl with 10 mM MgCl2, 2 mM ATP and 0.25 mM choline, pH 7.4, at 37°C

671362

0.0045

-

pH 9.0

0.119

-

0.169

-

1.5

-

10.67

-

2 microgram of purified protein is incubated with a reaction mixture of 100 mM MOPS (pH 7.8), 6 mM MgCl2 and 5 mM ATP, with either 2 mM ethanolamine and 200 nanoCi of [3H]ethanolamine or 2 mM choline and 200 nanoCi of (3H)choline at 37°C for 20 min and quenched by boiling at 100°C for 5 min. Substrates and products are separated by high-performance TLC using silica 60 plates with methanol/0.6% NaCl/ammonium hydroxide as solvent. Radiolabelled species are detected by fluorography at -70°C.

10.8

recombinant protein

143

-

pH 8.5, 37°C

641368, 641370

17.9

-

2.4

-

isozyme CKB-2, pH 10.0, 37°C

40.4

43

-

isozyme CKA-2, pH 10.0, 37°C

additional information

10

10.5

-

6.5

-

ADP + O-phosphocholine

7

assay at

7.4

-

assay at

671362

7.5

7.8

-

The pH optimum is assessed by measuring choline kinase activities at various pH values from pH 5.0 to pH 9.0

8

8 - 9.5

8.5

-

8.5 - 9

-

8.7

-

8.8

9

9.2

-

9.2 - 9.6

-

9.5

10.5

-

increase of activity up to

7.5 - 10

-

7.5 - 9

-

pH 7.5: about 30% of maximum activity, pH 9.0: about 45% of maximum activity

8.5 - 10.5

-

about 80% of maximum activity at pH 8.5 and pH 10.5

25

30

37

10

-

isoelectric focusing, basic isoform

641385

4.1

-

isoelectric disc gel electrophoresis, isoenzyme C

4.7 - 4.8

4.8

-

isoelectric focusing, isoform CKI

641370

5

-

isoelectric disc gel electrophoresis, isoenzyme B

Arabidopsis thaliana Col-0

-

Q8L518, Q9M9H6, Q9SZ92

UniProt

-

-

canola

-

-

641375, 641384, 662203, 663274, 673093, 673201

-

-

-

African green monkey

-

pigeon

-

-

641350, 641358

-

-

-

IFO 0987

Duttaphrynus melanostictus

-

toad

-

chicken

-

soy bean

-

Haemophilus influenzae

-

P14181

UniProt

Haemophilus influenzae ATCC BAA-255

-

Leishmania infantum JPCM5

P14181

UniProt

Haemophilus influenzae R6

-

UniProt

-

-

lizard

-

Heteropneustes fossilis

catfish

-

-

UniProt

Hoplobatrachus tigerinus

frog

-

-

-

-

UniProt

-

UniProt

-

-

-

-

-

-

-

UniProt

-

-

Saccharomyces cerevisiae KS106

-

641351, 641361, 641363, 641374, 641376, 641377, 663274, 673201, 674456, 687686

-

-

Schizosaccharomyces pombe

-

-

-

-

739407, 759237, 760133

Streptococcus pneumoniae ATCC BAA-255

UniProt

-

UniProt

-

-

protozoan parasite which causes African sleeping sickness

-

-

-

-

-

IBEC (CC-2541), primary bronchial epithelial cell

-

breast adenocarcinoma cell

-

cervical adenocarcinoma cell

-

-

colonic adenocarcinoma cell

-

-

colorectal cancer cell

-

egg

epidermoid carcinoma cell

-

-

-

-

-

-

-

-

-

-

Hepa-1

-

-

CC-2551, primary mammary epithelial cell

-

-

-

-

-

-

lactating

-

-

-

-

-

-

of the intestine

-

-

non-small cell lung cancer epithelial cell line

688743

NCI-H460 cell

-

non-small cell lung cancer epithelial cell line

688743

NCI-H510 cell

-

small cell lung cancer cell line

688743

NCI-H82 cell

prostate gland cancer cell

-

small cell lung cancer cell line

-

-

-

-

-

squamous cell carcinoma cell

-

-

umbilical vein endothelial cell

-

-

641358

yeast form

-

strains W303-1A,DY1457, ZHY6, ZHY3, SH304, SH303, SH307

687686

additional information

endoplasmic reticulum

-

-

isoform CKalpha

additional information

-

nuclear fraction

-

641358

Highest Expressing Human Cell Lines

Filter by:

Cell Line Links

Gene Links

evolution

malfunction

metabolism

physiological function

18 entries

additional information

29 entries

12750

-

4 * 12750

13000

-

4 * 13000

14400

-

x * 14400, basic isoform

641385

160000

-

gel filtration

641368, 641370

40600

-

isoform CKB-2: x * 40600, SDS-PAGE, x * 42000, deduced from gene sequence

42000

44000

45000

47000

-

4 * 47000, SDS-PAGE

641368, 641370

48000

-

SDS-PAGE

672898

48600

-

isoform CKA-2: x * 48600, SDS-PAGE, x * 49000, deduced from gene sequence

49000

-

isoform CKA-2: x * 48600, SDS-PAGE, x * 49000, deduced from gene sequence

50000

51000

52000

52070

-

calculation from amino acid sequence

641353

52200

-

calculated from amino acid sequence

53000

-

x * 53000, the parasite has two potential 53000 and 44000 Da isoforms, SDS-PAGE

56000

-

SDS-PAGE, recombinant protein

66000

-

1 * 66000

66300

67000

-

gel filtration

70000

-

x * 70000, full-length enzyme, SDS-PAGE

72610

-

determined by MALDI-TOF-MS

73000

75000 - 80000

87600

-

sucrose density gradient centrifugation, gel filtration

94000

-

?

dimer

homodimer

homotetramer

monomer

oligomer

tetramer

additional information

-

active form of enzyme consists of alpha/beta hetero-oligomers with small parts of activity expressed by alpha/alpha or beta/beta homo-oligomers

641378

phosphoprotein

Q9Y259

choline kinase beta is phosphorylated by protein kinase A

739447

additional information

-

enzyme activity is regulated via phosphorylation at S30 and/or S85 by protein kinase A

-

-

homodimer

-

641384

-

-

in complex with inhibitor V-11-023907, hanging drop vapor diffusion method, using 0.1 M Bis-Tris (pH 6.5), 25% (w/v) polyethylene glycol 3350, and 0.1 M MgCl2

721743

in complex with inhibitors, hanging drop vapor diffusion method, using 10-30% (w/v) polyethylene glycol 5000 monomethyl ether and 0.2 M magnesium phormate

isoform ChoKalpha1 in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M HEPES (pH 7.5), 25% (w/v) polyethylene glycol 3350, and 0.2 M lithium sulfate

isoform ChoKbeta in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M sodium cacodylate (pH 6.5), 30% polyethylene glycol 4000, and 0.2 M ammonium sulfate

purified choline kinase catalytic domain of the protein, residues 80-457, and of SH3-ChoKalpha1(60-69) fusion protein, from 0.2 M zinc acetate, 0.1 M imidazole pH 8.0, and 20% w/v PEG 3000, drops of 0.002 ml protein at 10 mg/ml are set at a 1:1 ratio with reservoir solution, 2-3 weeks, X-ray diffraction structure determination and analysis at 1.5 A resolution, structure modeling using the structure of c-Src-SH3 with the NS5A peptide, PDB ID 4QT7, as a model

purified recombinant isozyme ChoKalpha truncated mutant DELTA79 in apoform and in complex with inhibitor TCD-717, sitting drop vapor diffusion method, mixing of 0.002 ml of 10 mg/ml protein solution with 0.002 ml of reservoir solution containing 0.1 M MES, pH 6.5, and 20% PEG 3350, 2-3 days, 20°C, crystals are soaked with TCD-717 by mixing a 50 mM solution of 100% DMSO-resuspended compound in a 1:4 ratio with the reservoir buffer, X-ray diffraction structure determination and analysis at 2.35 A resolution

purified recombinant tagged enzyme in apoform and in complex with inhibitor 1-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]methanamine, mixing of 30 mg/ml protein solution with 0.1 M sodium formate, 8-12% PEG 3350 at 18°C, complex structures are obtained by soaking the inhibitors into the ChoKalpha1 crystals at a final concentration of 2-5 mM for 45-60 min before freezing in liquid nitrogen, X-ray diffraction structrue determination and analysis, modelling

sitting drop vapor diffusion method, using 20% (w/v) polyethylene glycol 3350 and 0.25 M potassium isothiocyanate

sitting drop vapour diffusion using 25 mM Tris/HCl (pH 7.5), 25 mM KCl, 0.5 mM dithiothreitol, 0.0005 ml of 0.1 M MgCl2 in 12-20% PEG 3350 with 0.2 M NaF

675410

purified recombinat His6-tagged choline kinase in apoform and in ADP-bound form, hanging drop vapor diffusion method, mixing of 0.001 ml of 10 mg/ml protein solution with 0.001 ml of reservoir solution, and equilibration against 0.5 ml reservoir solution, containing 16% v/v PEG 8000, 0.2 M NaCl, 0.1 M HEPES, pH 7.5, 2 mM Tris(2-carboxyethyl)phosphine (TCEP), and 4 mM MgCl2 for the apoform crystals, and the same composition with 2 mM ADP for the complex crystals, at room temperature, X-ray diffraction structrue determination and analysis at 2.0-2.2 A resolution, molecular replacement and model building using the PDB ID 3FI8 structure as starting model

759092

-

native and selenomethionine-labelled enzyme, hanging drop vapor diffusion method, using 0.1M HEPES, pH 7.5, 1.2 M sodium citrate and 4% (v/v) glycerol

moe

C252S

-

slightly increased turnover

D255A

D255E

D255N

D301A

D301E

D301N

D313A

-

low expression level

E125A

E125D

E125Q

E134A

-

slightly increased turnover

E151A

-

slightly increased turnover

E303A

E303D

E303N

-

small reduction of kcat

E303Q

-

reduced activity

E320A

H181A

-

low expression level

H253A

N254A

-

similar initial activity like wild type enzyme, but time instability

N260A

N308 A

-

small reduction of kcat

N308A

-

reduced activity

N308D

N308Q

N354A

-

strongly reduced activity, only minor effect on Km for both substrates

N87A

R111A

R149A

R149K

-

slightly increased turnover

S85T

-

reduced activity

S86A

S86T

-

moderate reduction of the catalytic efficiency

W387A

D255A

-

complete loss of activity

D306A

E125A

E255A

-

almost complete loss of activity

E303A

-

10fold decrease in activity

E320A

-

26fold higher Km for ATP

F352A

the mutant exhibits a higher turnover number compared to the wild type enzyme

F352L

the mutant exhibits a higher turnover number compared to the wild type enzyme

L401A

the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme

L401F

the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme

N255A

-

complete loss of activity

P59A/P60A

site-directed mutagenesis

P61A/P62A

site-directed mutagenesis

P72A/P73A

site-directed mutagenesis

R111A

-

2-25% catalytic efficiency compared to the wild type enzyme

S39D/S40D

Q9Y259

the choline kinase beta phosphorylation mimic behaves kinetically like the wild type enzyme

739447

S86A

-

2-25% catalytic efficiency compared to the wild type enzyme

W387A

-

2-25% catalytic efficiency compared to the wild type enzyme

Y197/333F

the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enzyme

Y197F

the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enzyme

Y333F

the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enzyme

S25A

-

mutation results in 32% decrease of phosphatidylcholine synthesis compared to the wild type enzyme

S25D

-

mutation results in 14% increase of phosphatidylcholine synthesis compared to the wild type enzyme

S30A

-

specific activity reduced by 44%, phosphorylation reduced by 70%

S30A/S85A

-

specific activity reduced by 60%, phosphorylation reduced by 83%

S85A

-

specific activity reduced by 8%, phosphorylation reduced by 17%

Saccharomyces cerevisiae KS106

S25A

-

mutation results in 32% decrease of phosphatidylcholine synthesis compared to the wild type enzyme

-

S25D

Saccharomyces cerevisiae KS106

-

mutation results in 14% increase of phosphatidylcholine synthesis compared to the wild type enzyme

-

D167A

the mutant shows about 14% activity compared to the wild type enzyme

T29A

the mutant shows about 10% activity compared to the wild type enzyme

T29S

the mutant shows slightly increased activity compared to the wild type enzyme

additional information

5

-

or below, 2-3 h, 90% or more loss of activity, crude enzyme extract

5.5 - 10

-

inactivation below and above

641351

30

-

40 min, without Mg2+, 80% loss of activity, + 15 mM Mg2+, 9% loss of activity

39

-

10 min, 15 mM Mg2+, 50% loss of activity

choline, ATP, bovine serum albumin and changes in ionic strength do not contribute to the stability of choline kinase

-

loss of activity upon freezing and thawing

-

very stable, even at a low protein concentration, 0.001 mg/ml

-

-18°C, enzyme kept frozen for 3 h and thawed, 15 min in contact with ice, complete inactivation, cannot be reactivated

-

-20°C, 50 mM Tris and 50 mM glycine pH 9.0, 24 h, 30-50% loss of activity

-20°C, stable without any stabilizing additives

-

641372

-80°C, 50 mM Tris and 50 mM glycine pH 9.0, with or without freeze drying, 24 h, about 50% loss of activity

0°C, 10 mM Tris actetate, pH 7.2, 13 mM 2-mercaptoethanol, 1 mM EGTA, 15 mM MgCl2, stable for 1 week

-

4°C, 50 mM Tris and 50 mM glycine pH 9.0, 24 h, no loss of activity

4°C, stable for at least 1 month

-

641371

-

7 entries

cleared lysate is applied to a HisTrap column column pre-loaded with Ni2+. Unbound proteins are removed by washing the column with 50 mM Tris/HCl, pH 8.0, 300 mM NaCl and 10 mM imidazole, whereas TbC/EK1 and TbC/EK2 are eluted with an imidazole gradient in the same buffer. Fractions containing TbC/EK1 or TbC/EK2 are pooled, dialysed against 50 mM Tris/HCl and 300 mM NaCl and purified further through a Superdex 200 16/60 gel-filtration column.

-

Con A column chromatography, Affi-Gel Blue gel filtration and Mono Q column chromatography

-

copurification of choline kinase and ethanolamine kinase

-

641345

glutathione affinity column chromatography, Ni-NTA column chromatography, and Superdex 200 gel filtration

721743

gluthatione-Sepharose column chromatography, Resource Q column chromatography and Superdex-200 gel filtration

675410

HisTrap column chromatography and Superdex 200 gel filtration

isoforms CKA-2, CKB-2

-

isoforms: CK I, CK II

-

multiple forms

-

Ni-nitrilotriacetic acid agarose affinity and gel filtration

-

Ni-NTA agarose resin column chromatography and 300SW gel filtration

-

Ni-NTA column chromatography

-

Ni-NTA column chromatography and Superdex 200 gel filtration

Ni-NTA resin column chromatography

overexpressed PfCK protein is purified to homogeneity using Ni-nitrilotriacetic acid agarose affinity and gel filtration chromatography

-

overview

partial

recombinant enzyme sChoK from Escherichia coli strain BL21(DE3)

760133

recombinant enzyme, from Sf-9 insect cells

-

641377

recombinant enzymes using His-tag

-

recombinant His-SUMO-tagged wild-type and mutant enzymes from Escherichia coli strain Rosetta (DE3)pLysS by nickel affinity chromatography, and dialysis, if necessary the tag is cleaved, followd by another nickel affinity chromatography step, and dialysis, the last step for all is gel filtration

recombinant His-SUMO-tagged wild-type and mutant enzymes from Escherichia coli strain Rosetta (DE3)pLysS by nickel affinity chromatography, and dialysis, if necessary the tag is cleaved, followed by another nickel affinity chromatography step, and dialysis, the last step for all is gel filtration

recombinant N-terminally His6-tagged enzyme from Escherichia coli strain BL21(DE3) Star by nickel affinity chromatography and gel filtration

759092

recombinant proteins using GST-tag

-

663274

recombinant tagged choline kinase alpha1 residues 75-457 by affinity and ion exchange chromatography, and gel filtration

two isoforms with greatly different pI

-

-

7 different genes, cloned 5

-

A mouse embryonic stem cell line (XH252, strain 129/OlaHsd) with an insertional mutation in choline kinase alpha is created in a gene-trapping prgram. The vector, pGT1Lxf, is designed to create an in-frame fusion between the 5' exons of the trapped gene and a reporter, betageo (a fusion of beta-galactosidase and neomycin phosphotransferase 2). CK-alpha spans 12 exons on mouse chromosome 19. The insertional mutation in XH252 occurred in intron 5. Thus, the gene-trapped locus is predicted to yield a fusion transcript containing exons 1-5 of CK-alpha and betageo. The embryonic stem cells are injected into C57BL/6 blastocysts to create chimeric mice, which are bred with C57BL/6 mice to generate heterozygous (+/-) CK-alpha-deficient mice. All mice had a mixed genetic background. The mice are weaned at 21 days of age, housed in a barrier facility with a 12-h light-dark cycle, and fed chow containing 4.5% fat. Creating of mice lacking CK- alpha with an embryonic stem cell line containing an insertional mutation in the gene for CK-alpha. Embryos homozygous for the mutant CK-alpha allele are recovered at the blastocyst stage, but not at embryonic day 7.5, indicating that CK-alpha is crucial for the early development of mouse embryos.

-

687709

a series of luciferase vectors that contained the CKalpha promoter and ranged from +57 to -3840 bp is constructed. The vectors are cotransfected into hepa-1 cells with the renilla luciferase expression vector as a control

O54804

685337

encoding isozymes alpha, beta

O54804

641383

enzyme cloned by complementation of the yeast choline kinase mutation cki

-

641353

enzyme expressed in Escherichia coli

-

641352

expressed in COS-7 cells

-

672371

expressed in Escherichia coli

expressed in Escherichia coli BL21(DE3) cells

expressed in Escherichia coli BL21DE3pLysS

Histophilus somni

B0URY8

705538

expressed in Escherichia coli Rosetta cells and in Saccharomyces cerevisiae KS106 cells

-

expressed in Escherichia coli strain BL21(DE3)

675410

expressed in Sf9 cells

-

expression in COS-7 cells

-

672371

gene CHKA, recombinant expression of His-SUMO-tagged wild-type and mutant enzymes in Escherichia coli strain Rosetta (DE3)pLysS

760183, 758809

gene CK1, recombinant overexpression in Arabidopsis thaliana plants via Agrobacterium tumefaciens-mediated transformation, quantitative RT-PCR enzyme expression analysis at normal or tunicamycin (Tm)-induced endoplasmic reticulum (ER) stress conditions

Q9M9H6, Q8L518, Q9SZ92

gene licA, recombinant expression of enzyme sChoK in Escherichia coli strain BL21(DE3)

760133

gene licA, sequence comparison of Streptococcus pneumoniae and human enzymes, overview

His-tag, expressed in Escherichia coli BL21(DE3)-pRIL

locus At1g74320, recombinant overexpression in Arabidopsis thaliana plants via Agrobacterium tumefaciens-mediated transformation, quantitative RT-PCR enzyme expression analysis at normal or tunicamycin (Tm)-induced endoplasmic reticulum (ER) stress conditions

Q9M9H6, Q8L518, Q9SZ92

locus At4g09760, recombinant overexpression in Arabidopsis thaliana plants via Agrobacterium tumefaciens-mediated transformation, quantitative RT-PCR enzyme expression analysis at normal or tunicamycin (Tm)-induced endoplasmic reticulum (ER) stress conditions

Q9M9H6, Q8L518, Q9SZ92

molecular cloning and recombinant expression in Escherichia coli strains DH5alpha, XL-1 blue and TOP10. BL21-Gold(DE3) is used for protein overexpression, RNA from bloodstream form of Trypanosoma brucei is used for cDNA synthesis.

-

native and mutant enzymes expressed as His-tag fusion protein in Sf9 cells

-

overview

parts of the alpha and beta subtype expressed as GST-fusion protein in Escherichia coli, alpha and beta subtype coexpressed in COS-7 cells

-

663274

plasmid maintenance and amplification are performed in Escherichia coli strain DH5 alpha

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687686

recombinant expression of N-terminally His6-tagged enzyme in Escherichia coli strain BL21(DE3) Star

759092

recombinant expression of tagged choline kinase alpha1 residues 75-457

Small interfering RNA-chk (siRNA) is designed and transfected for 48 h using oligofectamine and Opti-MEM based on the observed decrease of Chk message using reverse transcription-PCR analysis within this time. Immunoblot assay results with Chk antibody shows significant reduction of Chk protein expression levels in MCF-12A, MCF-7, and MDA-MB-231 cells after transient siRNA-chk transfection.

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685941

The genomic sequence of the putative human chk-alpha promoter is obtained by performing a BLAST search in National Center for Biotechnology Information using the known promoter sequence of the rat chk-a gene as query sequence. A 2.3-kb region at the 5'-end of the human chk-a gene on chromosome 11, immediately upstream of the translation start site, is found to contain several putative HRE sites with the core sequence RCGTG. Due to its high GC content, this 2.3-kb region is cloned as four smaller overlapping fragments, and formamide (5%) is added in all PCRs. The four overlapping sequences are PCR amplified from human genomic DNA. The PCR products of paired sense and antisense primer sequences used for the cloning of these fragments (Chk) are subcloned into the pCR 2.1 TA vector. The full 2.3-kb promoter region is obtained by appropriate endonuclease digestions and ligation of these four overlapping fragments. Each of the four fragments alone, as well as several subligations of two or three consecutive fragments, and the full-length 2.3-kb chk-a promoter are cloned into the pGL4-basic Luc reporter vector.

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685954

The RT-PCR-amplified PfCK gene is cloned in pRSET-C, an Escherichia coli expression vector. The host strain is optimized

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To identify the region of the CK apha promoter that is important to regulate its transcription, a series of luciferase vectors that contained the CK alpha promoter and ranged from +57 to -3840 bp are constructed. The vectors are cotransfected into Hepa-1 cells with the renilla luciferase expression vector as a control

O54804

685337

Transfection of human HeK293T is carried out by the calcium phosphate method. The amount of plasmidic DNA is kept constant at 0.2 mg with the corresponding empty vector. Tumors induced by ChoK alpha over-expression in Hek293T are removed from the mice to generate the ChoK tumoral cell line ADJ. Different slices of the tissue are placed into culture 100mm dishes and treated with trypsin and G418 to avoid murine cells contamination. The resultant cell line (ADJ) displays constitutive ChoK alpha activation and a fully transformed phenotype

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687121

choline kinase activity and expression in MG-63 cells are significantly higher than those in primary human osteoblasts

737751

choline kinase activity in forelimb and hindlimb muscle decreases with increasing age from 1 to 8 weeks

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721704

expression levels increase with increasing malignancy of the cell lines, i.e., MDA-MB-231 > MCF-7 > MCF-12A